Synthesis and in-vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid

Yousefi, Samira and Bayat, Saadi and Abdul Rahman, Mohd Basyaruddin and Ibrahim, Zalikha and Abdulmalek, Emilia (2017) Synthesis and in-vitro bioactivity evaluation of new galactose and fructose ester derivatives of 5-aminosalicylic acid. Chemistry & Biodiversity, 14 (4). e1600362-1. ISSN 1612-1880

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Abstract

Inflammatory bowel disease (IBD) is the main risk factor for developing colorectal cancer which is common in patients of all ages. 5-aminosalicylic acid (5-ASA), structurally related to the salicylates, is highly active in the treatment of IBD with minor side effects. In this study, the synthesis of galactose and fructose esters of 5-ASA was planned to evaluate the role of glycoconjugation on the bioactivity of the parent drug. The antibacterial activity of the new compounds were evaluated against two Gram-negative and two Gram-positive species of bacteria, with a notable effect observed against Staphylococcus aureus and Escherichia coli in comparisons with the 5-ASA. Cytotoxicity testing over HT-29 and 3T3 cell lines indicated that the toxicity of the new products against normal cells was significantly reduced compared with the original drug, whereas their activity against cancerous cells was slightly decreased. The anti-inflammatory activity test in RAW264.7 macrophage cells indicated that the inhibition of nitric oxide by both of the monosaccharide conjugated derivatives was slightly improved in comparison with the non-conjugated drug.

Item Type:	Article (Journal)
Additional Information:	7854/57352
Uncontrolled Keywords:	5-ASA, Galactose, Fructose, Biological evaluation
Subjects:	Q Science > QD Chemistry
Kulliyyahs/Centres/Divisions/Institutes (Can select more than one option. Press CONTROL button):	Kulliyyah of Pharmacy > Department of Pharmaceutical Chemistry
Depositing User:	Asst. Dr. Zalikha Ibrahim
Date Deposited:	21 Jun 2017 10:44
Last Modified:	09 Mar 2018 15:08
URI:	http://irep.iium.edu.my/id/eprint/57352

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